Abstract

The invention discloses species compounds (4) and (5) and methods of using these compounds for therapeutically treating a patient for an illness selected from the group consisting of infection by Pneumocystis carinii and Toxoplasmosis gondii. ##STR1## In compounds (4) and (5) X and Y may be the same or different and are selected from the group consisting of OH and NH.sub.2 : A is selected from the group consisting of nitrogan, carbon and sulfur and B equals carbon when A is selected from the group consisting of sulfur, carbon and nitrogen, B equals nitrogen when A equals carbon and B equals sulfur when A equals carbon; R.sub.3 is one of either hydrogen or methyl except when attached to Nitrogen wherein R.sub.3 is zero; R.sub.4 is one of either a hydrogen or a first lower alkyl group except when A equals sulfur wherein R.sub.4 is zero; R.sub.1 is selected from the group consisting of hydrogen, nitroso group, aldehyde, a second lower alkyl group except when B is equal to sulfur wherein R.sub.1 is zero; and R.sub.2 is selected from the group consisting alkyl, dialkyl and trialkyl groups, alkylaryl, diaryl and triaryl groups, substituted aryl, diaryl and triaryl groups, an alkoxy, substituted alkoxy and halogen.

Claims

1. A compound and pharmaceutically acceptable salts having the species formula (4) ##STR23## wherein X and Y may be the same or different and are selected from the group consisting of OH and NH.sub.2, wherein A is selected from the group consisting of nitrogen, CH and sulfur and B equals CH when A is selected from the group consisting of sulfur, CH and nitrogen or B equals nitrogen when A equals CH or B equals sulfur when A equals CH wherein R.sub.3 is zero; wherein R.sub.4 is one of either a hydrogen or a first lower alkyl group except where A equals sulfur wherein R.sub.4 equals zero; wherein R.sub.1 is selected from the group consisting of hydrogen, a nitroso group, a formyl group, a second lower alkyl group which is the same or different than the first lower alkyl group except when B is equal to sulfur, wherein R.sub.1 is equal to zero; and wherein R.sub.2 is selected from the group consisting of a third lower alkyl group which is the same or different than the first lower alkyl group and the second lower alkyl group, an aryl group, an alkylaryl group, a substituted aryl group, a substituted alkylaryl group, a diaryl group, a triaryl group, an alkyldiaryl group, an alicyclic hydrocarbon group, an alkyltriaryl group, a substituted diaryl group, and a substituted triaryl group, and each substituent of the substituted aryl group, diaryl group, triaryl group, or the substituted alkylaryl group, alkyldiaryl group, alkyltriaryl group is the same or different and is selected from the group consisting of a fourth lower alkyl group which is the same as or different than the first lower alkyl group, the second lower alkyl group, the third lower alkyl group, an alkoxy, a substituted alkoxyaryloxy group and a halogen.

2. The compound and pharmaceutically acceptable salts of claim 1 wherein said first lower alkyl group has one to about six carbon atoms branched, unbranched and alicyclic, said second lower alkyl group has one to about six carbon atoms branched, unbranched and alicyclic and said third lower alkyl group has one to about six carbon atoms branched, unbranched and alicyclic; wherein said alkylaryl group is selected from the group consisting of an alkylphenyl and alkylbenzyl group; wherein said alkyldiaryl group is selected from the group consisting of alkylnaphthyl, alkylbenzothiophene, alkylindene, alkylbenzofuran, alkylindole, and alkylaminoquinoline; wherein alkyltriaryl group is an alkylanthracyl group; wherein said substituted aryl group, diaryl group and triaryl group is selected from the group consisting of a mono-, di- and tri-substituted aryl group, diaryl group and triaryl group; wherein said substituted alkylaryl group is selected from the group consisting of mono-, di- and tri-substituted alkylphenyl and alkylbenzyl group; wherein each substituted alkyldiaryl and alkyltriaryl group is selected from the group consisting of a mono-, di- and tri-substituted alkylnaphthyl, alkylbenzothiophene, alkylindole, alkylbenzofuran, alkylindine, alkylaminoquinoline and alkylanthracyl group and wherein each substituent is the same or different and is selected from the group consisting of methyl, ethyl, n-propyl, n-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, methoxy group, chlorine atom, bromine atom and fluorine atom.

3. The compound and pharmaceutically acceptable salts of claim 1 wherein X and Y are each NH.sub.2, R.sub.2 is zero, R.sub.2 is 2',5'-dimethoxyphenyl, R.sub.3 is zero, R.sub.4 is hydrogen, A is CH and B is sulfur.

4. The compound and pharmaceutically acceptable salts of claim 1 wherein X and Y are each NH.sub.2, R.sub.1 is hydrogen, R.sub.2 is 2',5'-dimethoxyphenyl, R.sub.3 is zero, R.sub.4 is CH.sub.3, A is nitrogen and B is CH.

5. The compound and pharmaceutically acceptable salts of claim 1 wherein X and Y are each NH.sub.2, R.sub.1 is hydrogen, R.sub.2 is 3',4',5'-trimethoxyphenyl, R.sub.3 is zero, R.sub.4 is hydrogen, A is CH and B is CH.

6. The compound and pharmaceutically acceptable salts of claim 1 wherein X and Y are each NH.sub.2, R.sub.1 is hydrogen, R.sub.2 is 1'naphthyl, R.sub.3 is zero, R.sub.4 is hydrogen, A is nitrogen and B is CH.

7. A method of therapeutically treating a patient for an illness consisting of employing a compound and pharmaceutically acceptable salts thereof having the species formula (4) ##STR24## wherein X and Y may be the same or different and are selected from the group consisting of OH and NH.sub.2, wherein A is selected from the group consisting of nitrogen, CH and sulfur and B equals CH when A is selected from the group consisting of sulfur, CH and nitrogen or B equals nitrogen when A equals CH or B equals sulfur when A equals CH wherein R.sub.3 is zero; wherein R.sub.4 is one of either a hydrogen or a first lower alkyl group except where A equals sulfur wherein R.sub.4 equals zero; wherein R.sub.1 is selected from the group consisting of hydrogen, a nitroso group, a formyl group, a second lower alkyl group which is the same or different than the first lower alkyl group except when B is equal to sulfur, wherein R.sub.1 is equal to zero; and wherein R.sub.2 is selected from the group consisting of a third lower alkyl group which is the same or different than the first lower alkyl group and the second lower alkyl group, an aryl group, an alkylaryl group, a substituted aryl group, a substituted alkylaryl group, a diaryl group, a triaryl group, an alkyldiaryl group, an alkyltriaryl group, an alicyclic hydrocarbon group, a substituted diaryl group, and a substituted triaryl group, and each substituent of the substituted aryl group, diaryl group, triaryl group, or the substituted alkylaryl group, alkyldiaryl group, alkyltriaryl group is the same or different and is selected from the group consisting of a fourth lower alkyl group which is the same as or different than the first lower alkyl group, the second lower alkyl group, the third lower alkyl group, an alkoxy, a substituted alkoxyaryloxy group and a halogen;

which comprises:

incorporating said compound in a suitable pharmaceutical carrier;

administering a therapeutically effective amount of said compound incorporated in said carrier to a patient who is immunocompromised; and

employing said method in therapeutically treating a patient for an illness selected from the group consisting of infection by Pneumocystis carinii and Toxoplasmosis gondii.

8. The method of claim 7 including employing said carrier selected from the group consisting of physiologic saline and 5% dextrose for injection.

9. The method of claim 7 including administering said compound incorporated in said carrier to a patient by the parenteral route.

10. The method of claim 7 including administering said compound incorporated in said carrier to a patient by the oral route.

11. The method of claim 7 including administering said compound incorporated in said carrier to a patient topically.

12. A method of prophylactically administering to a patient a compound and pharmaceutically acceptable salt thereof having the species formula (4) ##STR25## wherein X and Y may be the same or different and are selected from the group consisting of OH and NH.sub.2 wherein A is selected from the group consisting of nitrogen, CH and sulfur and B equals CH when A is selected from the group consisting of sulfur, CH and nitrogen or B equals nitrogen when A equals CH or B equals sulfur when A equals CH wherein R.sub.3 is zero; wherein R.sub.4 is one of either a hydrogen or a first lower alkyl group except where A equals sulfur wherein R.sub.4 equals zero; wherein R.sub.1 is selected from the group consisting of hydrogen, a nitroso group, a formyl group, a second lower alkyl group which is the same or different than the first lower alkyl group except when B is equal to sulfur, wherein R.sub.1 is equal to zero; and wherein R.sub.2 is selected from the group consisting of a third lower alkyl group which is the same or different than the first lower alkyl group and the second lower alkyl group, an aryl group, an alkyl aryl group, a substituted aryl group, a substituted alkylaryl group, a diaryl group, a triaryl group, an alkyldiaryl group, an alkyltriaryl group, an alicyclic hydrocarbon group, a substituted diaryl group, and a substituted triaryl group, and each substituent of the substituted aryl group, diaryl group, triaryl group, or the substituted alkylaryl group, alkyldiaryl group, alkyltriaryl group is the same or different and is selected from the group consisting of a fourth lower alkyl group which is the same as or different than the first lower alkyl group, the second lower alkyl group, the third lower alkyl group, an alkoxy, a substituted alkoxyaryloxy group and a halogen;

which comprises:

incorporating said compound in a suitable pharmaceutical carrier;

administering a prophylactically effective amount of said compound incorporated in said carrier to a patient who is immunocompromised; and

employing said method in prophylactically treating a patient to provide protection against an illness selected a group consisting of infection by Pneumocystis carinii and Toxoplasmosis gondii.

13. The method of claim 12 including employing said carrier selected from the group consisting of physiologic saline and 5% dextrose for injection.

14. The method of claim 12 including administering said compound incorporated in said carrier to a patient by the parenteral route.

15. The method of claim 12 including administering said compound incorporated in said carrier to a patient by the oral route.

16. The method of claim 12 including administering said compound incorporated in said carrier to a patient topically.